[^(99)Tc^mN(PNP5)(DTC)]^+混配配合物的合成及其在小鼠体内的生物分布  

Synthesis and Biodistribution in Mice of [^(99)Tc^mN(PNP5)(DTC)]^+ Heterocomplexes

作　　者：楚进锋[1] 王学斌[2] 

机构地区：[1]北京化工大学化工资源有效利用国家重点实验室,北京100029 [2]北京师范大学化学学院放射性药物教育部重点实验室,北京100875

出　　处：《同位素》2009年第2期101-105,共5页Journal of Isotopes

基　　金：北京化工大学青年教师自然科学研究基金资助项目(QN0624)

摘　　要：通过配体交换反应制备了4种脂溶性阳离子配合物:[99TcmN(PNP5)(PODC)]+(PNP5:N,N-二[二(3-甲氧基丙基)膦基乙基]-2-乙氧基乙胺;PODC:N-甲氧基氨荒酸盐)、[99TcmN(PNP5)(BODC)]+(BODC:N-乙氧基氨荒酸盐)、[99TcmN(PNP5)(MOPDTC)]+(MOPDTC:N-甲氧基丙基氨荒酸盐)和[99TcmN(PNP5)(EOPDTC)]+(EOPDTC:N-乙氧基丙基氨荒酸盐),放化纯度均大于90%。小鼠生物分布结果显示:4种配合物在小鼠体内均有不同程度的心肌摄取和滞留,主要经肾排泄,在血、肝和肺等非靶组织中清除较快。其中,[99TcmN(PNP5)(EOPDTC)]+的靶与非靶组织放射性摄取比(T/NT)较高,30 min时,心脏与血、心脏与肺及心脏与肝的T/NT分别为23.75、3.45和3.63,利于快速心肌显像。若能通过结构修饰提高其心肌摄取,有望发展为一种新型心肌灌注显像剂。[^99Tc^mN（PNP5）（DTC）]^＋ （ PNP5 ： bis （dimethoxypropylphosphinoethyl） etho xyethylamine, PODC： N-methoxyethyl dithioearbamate）, [^99Tc^mN（PNP5）（BODC）]^＋ （BODC： N-ethoxyethyl dithioearbamate）, [^99Tc^mN（PNP5）（MOPDTC）]^＋ （ MOPDTC： N- methoxypropyl dithioear-bamate） and [^99Tc^mN（PNP5）（EOPDTC）]^＋ （EOPDTC： N- ethoxypropyl dithioearbamate） four 99 Tem-nitride heteroeomplexes were synthesized by lig-and exchange reaction. They were lipophilie cations with good stability, and their radiochemical purities were over 90%. The results of biodistribution in mice showed that the four heterocomplexes had different degrees of myocardial uptake and retention, and could be washed out rapidly from blood, liver, lungs and other non-target tissues, and were mainly eliminated through kidneys. Among the four complexes, the uptake ratios of heart to blood, heart to lung and heart to liver at 30 min of [^99Tc^mN（PNP5）（EOPDTC）]^＋ were 23. 75, 3.45, 3. 63, and it was conductive to rapid cardiac imaging, respecinely. It could be developed a novel myocardial perfusion imaging agent by structural optimization to improve its myocardial uptake.

关 键 词：[99TcmN(PNP5)(DTC)]+ 混配配合物 心肌灌注显像剂 生物分布 

分 类 号：O615.4[理学—无机化学]